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Assay Detail

CHEMBL809254

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Binding
Ability to inhibit thymidylate synthase derived from human leukemia K562 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type K562
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Thymidylate synthase (CHEMBL1952)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Folate analogues as inhibitors of thymidylate synthase.
Brixner DI, Ueda T, Cheng YC, Hynes JB, Broom AD.
J Med Chem (1987) 30 : 675 -678
PubMed 3470522 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.77 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL389051 1 7.43
CHEMBL347223 1 6.54
CHEMBL348979 1 5.90
CHEMBL161457 1 5.62
CHEMBL158790 1 5.60
CHEMBL22973 1 5.57
CHEMBL350921 1 5.26
CHEMBL161265 1 4.26
CHEMBL1622 FOLIC ACID 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL389051 IC50 = 37.0 nM 7.43
CHEMBL347223 IC50 = 290.0 nM 6.54
CHEMBL348979 IC50 = 1260.0 nM 5.90
CHEMBL161457 IC50 = 2400.0 nM 5.62
CHEMBL158790 IC50 = 2500.0 nM 5.60
CHEMBL22973 IC50 = 2700.0 nM 5.57
CHEMBL350921 IC50 = 5500.0 nM 5.26
CHEMBL161265 IC50 = 55000.0 nM 4.26
CHEMBL1622 FOLIC ACID IC50 = 290000.0 nM -